Piperidine derivatives

US6166209A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Geo Adam · Schopfheim, DE
• Andrea Cesura · Nyon, CH
• Guido Galley · Rheinfelden (Baden), DE
• François Jenck · Riedisheim, FR
• Stephan Rover · Weil am Rhein, DE
• Jurgen Wichmann · Steinen, DE

Key dates

• Filing date: Nov 20, 1998
• Grant date: Dec 26, 2000
• Expiry date: Nov 20, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --; PA1 Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--; PA1 n is 1 or 2 or PA1 X and Y taken together are --CH.dbd.CH-- PA1 Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--; PA1 A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2; PA1 R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl; PA1 R.sup.3 is hydrogen or halogen; PA1 R.sup.4 is hydrogen or hydroxy and PA1 the dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na.sup.+ excretion and arterial blood pressure disord…